Mark P Fereshteh, Xin Li, Sha Li, Yi Fan, Rosemary Zhang, Glen A Farr, Garrett Kolodin, Jonathan Lippy, Joseph G Naglich, Gary Schieven, Liang Schweizer, Litao Zhang
Oral agents targeting Janus-associated kinases (JAKs) are promising new agents in clinical development. To better understand the relationship between JAK inhibition and biological outcome, compounds targeting JAKs were evaluated in peripheral human whole blood. To date, these analyses are low throughput and costly. Here, we developed a robust 384-well, high-throughput flow-based assay approach to screen small molecules for JAK/STAT signaling inhibition in human whole blood. This assay platform provides a highly sensitive analysis of signaling events in blood and facilitates measurement of target engagement...
September 2016: Journal of Biomolecular Screening